US4307110A
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Mercaptoacyl derivatives of 3-substituted proline derivatives
Assignee: ER Squibb and Sons LLC
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Filing: 1980-09-12
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Granted: 1981-12-22
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Expires: 2000-09-12
Abstract
Abstract New mercaptoacyl derivatives of 3-substituted proline derivatives are provided which have the general formula ##STR1## and are useful as hypotensive agents.
Inventors
- 👤 Michael E. Condon
- 👤 Miguel A. Ondetti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 11:47
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D207/18; C07D207/22; C07D207/24
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
122 words
A compound of the formula ##STR32## and physiologically acceptable basic salts thereof; X is SH, lower alkoxy, lower alkylthio, hydroxy, phenylthio, phenyloxy, biphenylthio, biphenyloxy, 1-naphthylthio, 1-naphthyloxy, 2-naphthylthio, 2-naphthyloxy, substituted phenylthio or substituted phenyloxy wherein the substituents on the above phenyl groups are one or two halogens, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro groups; R is hydrogen or lower alkyl; R 1 is hydrogen, hydroxy, halogen or lower alkoxy, with the proviso that when R 1 is hydrogen, X can only be SH, and R 1 and X cannot both be hydroxy; R 2 is hydrogen, lower alkyl or trifluoromethyl; R 3 is hydrogen, ##STR33## R 4 is lower alkyl or phenyl; and n is 0, 1 or 2.
Claim 2
Dependent Claim
122 words
A compound of the formula ##STR32## and physiologically acceptable basic salts thereof; X is SH, lower alkoxy, lower alkylthio, hydroxy, phenylthio, phenyloxy, biphenylthio, biphenyloxy, 1-naphthylthio, 1-naphthyloxy, 2-naphthylthio, 2-naphthyloxy, substituted phenylthio or substituted phenyloxy wherein the substituents on the above phenyl groups are one or two halogens, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro groups; R is hydrogen or lower alkyl; R 1 is hydrogen, hydroxy, halogen or lower alkoxy, with the proviso that when R 1 is hydrogen, X can only be SH, and R 1 and X cannot both be hydroxy; R 2 is hydrogen, lower alkyl or trifluoromethyl; R 3 is hydrogen, ##STR33## R 4 is lower alkyl or phenyl; and n is 0, 1 or 2.
Claim 3
Dependent Claim
9 words
The compound of claim 1 wherein X is SH.
Claim 4
Dependent Claim
18 words
The compound of claim 1 wherein R 1 is hydrogen, R 2 is hydrogen and n is 1.
Claim 5
Dependent Claim
10 words
The compound of claim 1 wherein R 3 is hydrogen.
Claim 6
Dependent Claim
13 words
The compound of claim 1 wherein the proline ring is in the L-configuration.
Claim 7
Dependent Claim
12 words
The compound of claim 1 wherein X is in the trans configuration.
Claim 8
Dependent Claim
22 words
The compound of claim 1 wherein X is SH, R 1 is hydrogen, R 2 is hydrogen and R 3 is hydrogen.
Claim 9
Dependent Claim
10 words
The compound of claim 1 having the name (trans) 3-mercapto-1-(3-mercapto-1-oxopropyl)proline.
Claim 10
Dependent Claim
24 words
A composition useful in the treatment of hypertension comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 11
Dependent Claim
21 words
A method for reducing blood pressure in hypertensive mammals which comprises administering an effective amount of the composition of claim 9.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-12-21 | 1985-06-22 | 1985-12-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-12-21 | 1989-06-22 | 1989-12-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-12-21 | 1993-06-22 | 1993-12-22 | $7700.00 | Window Closed / Lapsed |